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Assay Detail

CHEMBL4314367

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Wróbel MZ, Chodkowski A, Herold F, Marciniak M, Dawidowski M, Siwek A, Starowicz G, Stachowicz K, Szewczyk B, Nowak G, Belka M, Bączek T, Satała G, Bojarski AJ, Turło J.
Eur J Med Chem (2019) 183 : 111736 -111736
PubMed 31586817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.07 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1237021 LURASIDONE 4.0 1 9.30
CHEMBL2105760 BREXPIPRAZOLE 4.0 1 8.43
CHEMBL4483554 1 7.60
CHEMBL4571862 1 7.30
CHEMBL2028019 CARIPRAZINE 4.0 1 6.96
CHEMBL2377590 1 6.71
CHEMBL4591440 1 6.50
CHEMBL2377591 1 6.46
CHEMBL4454176 1 6.34
CHEMBL4571321 1 6.19
CHEMBL4515160 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1237021 LURASIDONE Ki = 0.5 nM 9.30
CHEMBL2105760 BREXPIPRAZOLE Ki = 3.7 nM 8.43
CHEMBL4483554 Ki = 25.0 nM 7.60
CHEMBL4571862 Ki = 50.0 nM 7.30
CHEMBL2028019 CARIPRAZINE Ki = 111.0 nM 6.96
CHEMBL2377590 Ki = 196.0 nM 6.71
CHEMBL4591440 Ki = 320.0 nM 6.50
CHEMBL2377591 Ki = 345.0 nM 6.46
CHEMBL4454176 Ki = 458.0 nM 6.34
CHEMBL4571321 Ki = 641.0 nM 6.19
CHEMBL4515160 Ki = 1158.0 nM 5.94